The present invention relates to new steroidal compounds which have valuable pharmacological properties.
For the treatment of certain forms of hypertonia, of edemas, of primary aldosteronism, and of other endocrinological imbalances caused by aldosterone, and for use as diuretics, compounds are utilized which reverse the effect of aldosterone or deoxycorticosterone on the excretion of sodium and potassium salts. These include as their most well-known representative the compound spironolactone, which has been available commercially for some time. However, frequently, undesirable endocrinic side effects occur in the treatment with spironolactone. These are evoked by the antiandrogenic and progestational activity of spironolactone. Thus, with a relatively long-term treatment of male patients with spironolactone, occurrence of gynecomastia is observed (Smith, W. G., The Lancet, 1962, p. 886; Mann, N. M., JAMA 1963, p. 778; Clark, E., JAMA 1965, p. 157; Greenblatt,t D. J., JAMA 1973, p. 82) and impotence is observed as well (Greenblatt, D. J., JAMA 1973, p. 82), due to the antiandrogenic side effect of this active agent (Steelman, S. L. et al., Steroids 1963, p. 449; Schane, H. P., J. of Clinical Endocrinology and Metabolism 1978, p. 691).
In contrast, the progestational side effect of spironolactone is blamed for secondary symptoms such as amenorrhea and cycle irregularities occurring in women when treated with spironolactone. Both side effects can be confirmed in animal experiments as well as in vitro by receptor binding tests with the androgen and progestogen receptor, respectively.